BPR1M492 is a brain-penetrant μ-opioid receptor ( MOR ) agonist an in vitro EC 50 of 0.93 nM in the cAMP inhibition assay and 0.004 nM in the FLIPR Ca 2+ assay without a clear signaling bias between cAMP and β-arrestin-2 pathway. BPR1M492 is a cAMP-biased nociceptin-orphanin FQ opioid peptide agonist. BPR1M492 is a weak cAMP-biased δ/κ-opioid receptor agonist. BPR1M492 demonstrates potent in vivo antinociception and can be used for pain research.
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